Investigation of spheronization mechanism of pharmaceutical drug crystals via mechanical powder processing

2020 Fiscal Year Final Research Report

• Project/Area Number: 18K14890
• Research Category: Grant-in-Aid for Early-Career Scientists
• Allocation Type: Multi-year Fund
• Review Section: Basic Section 47020:Pharmaceutical analytical chemistry and physicochemistry-related
• Research Institution: Meijo University
• Principal Investigator: Kondo Keita 名城大学, 薬学部, 助教 (90710913)
• Project Period (FY): 2018-04-01 – 2021-03-31
• Keywords: 無溶媒プロセス / 造粒 / 球形化 / 非晶質化 / 付着性 / 機械特性

Outline of Final Research Achievements

In this study, we investigated correlations between mechanical pelletization and physical characteristics (including crystal structure and mechanical properties) of drug crystals. At low temperatures, the surface of drug crystals was broken down under mechanical stress and became amorphous state. At middle temperatures, amorphized surface became sticky, resulting in agglomeration of drug crystals. At high temperatures, amorphous drug became deformable under mechanical stress and was spheronized.

Free Research Field

製剤学

Academic Significance and Societal Importance of the Research Achievements

本研究により，溶媒（水や有機溶媒を含む）を使用せず薬物結晶を球形化させるメカニズムを解明した．これらの知見は，溶媒を使用しない医薬品製造法の確立に寄与し，製造工程の短縮化や低コスト化により医薬品の低価格化，ひいては医療費の削減につながる．一方で，今回明らかにした機械的処理による結晶構造の変化は，非常に溶解しやすい非晶質医薬品を造粒・球形化させながら製造できる新たな製剤化技術の確立につながる．